作者
Lina Baranauskienė, Mika Hilvo, Jurgita Matulienė, Dmitrij Golovenko, Elena Manakova, Virginija Dudutienė, Vilma Michailovienė, Jolanta Torresan, Jelena Jachno, Seppo Parkkila, Alfonso Maresca, Claudiu T Supuran, Saulius Gražulis, Daumantas Matulis
发表日期
2010/12/1
期刊
Journal of enzyme inhibition and medicinal chemistry
卷号
25
期号
6
页码范围
863-870
出版商
Taylor & Francis
简介
The binding and inhibition strength of a series of benzimidazo[1,2-c][1,2,3]thiadiazole-7-sulphonamides were determined for recombinant human carbonic anhydrase isoforms I, II, and IX. The inhibition strength was determined by a stop-flow method to measure carbon dioxide hydration. Inhibitor-enzyme binding was determined by two biophysical techniques – isothermal titration calorimetry and thermal shift assay. The co-crystal structure was determined by X-ray crystallography. Comparing the results obtained using three different inhibition and binding methods increased the accuracy of compound affinity ranking and the ability to determine compound inhibitory specificity towards a particular carbonic anhydrase isoform. In most cases, all three methods yielded the same results despite using very different approaches to measure the binding and inhibition reactions. Some of the compounds studied are …
引用总数
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